Gastro-Resistant Bile Acid Sequestrant Tablets for Colon Targeting
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Solution Overview
Problem
Current bile acid sequestrants for treating bile acid malabsorption and diarrhea have issues with patient compliance due to high doses, adverse reactions, and negative drug interactions, as they are not specifically targeted to the colon and interfere with the natural digestive function of bile acids in the upper GI tract.
Innovation Solution
A pharmaceutical composition with a high drug load, formulated as a tablet core coated for gastro-resistant release in the ileum and colon, minimizing adverse reactions and interactions by targeting excess bile acids in the colon.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If high doses of bile acid sequestrants are administered to treat bile acid malabsorption, then therapeutic effectiveness is improved, but patient compliance deteriorates due to adverse reactions and negative drug interactions
Solution Approach 1:
The patent divides the treatment approach into targeted segments by using gastro-resistant formulations that release bile acid sequestrants specifically in the ileum and colon rather than throughout the entire GI tract. This segmentation allows effective bile acid binding in the target areas while preserving bile acid function in the upper GI tract, thereby maintaining therapeutic effectiveness while reducing adverse reactions and improving patient compliance
Solution Approach 2:
The patent applies local quality by creating formulations with different release characteristics tailored to specific GI locations. The gastro-resistant coating ensures drug release occurs only in the ileum and colon where excess bile acids are present, providing localized treatment that maintains system-wide bile acid homeostasis. This localized approach reduces systemic side effects while maintaining therapeutic effectiveness
2Reliability
If bile acid sequestrants are administered to sequester bile acids, then diarrhea is reduced, but adverse reactions and negative drug interactions increase
Solution Approach 1:
The patent extracts and removes excess bile acids specifically from the ileum and colon using targeted bile acid sequestrant release. By taking out only the excess bile acids in the lower GI tract while leaving bile acids intact in the upper GI tract, the formulation effectively controls diarrhea without causing the adverse reactions associated with systemic bile acid depletion or widespread drug interactions
Solution Approach 2:
The gastro-resistant coating acts as an intermediary that controls where and when the bile acid sequestrant becomes active. This intermediary mechanism ensures the drug only interacts with bile acids in the target areas (ileum and colon), preventing harmful interactions with other medications and reducing adverse reactions while still achieving effective diarrhea control
3Reliability
If conventional bile acid sequestrants are used, then bile acid binding occurs, but digestive function of bile acids in the upper GI tract is interfered with
Solution Approach 1:
The gastro-resistant coating performs preliminary protection of bile acids in the upper GI tract by preventing premature binding. The coating remains intact through the stomach and duodenum, allowing bile acids to perform their essential digestive functions undisturbed. Only after passing through the upper GI tract does the coating dissolve, allowing bile acid binding to occur in the ileum and colon where it is needed
Applied Scientific Principles
This section explains which scientific principles are used to turn an abstract innovation direction into a practical engineering solution.
Function Achieved in This Case
The formulation improves patient compliance by reducing the number of administrations and minimizes adverse effects, while effectively sequestering bile acids in the colon, thus reducing diarrhea and maintaining the digestive function of bile acids in the upper GI tract.
Implementation Method 1
A pharmaceutical composition with a high drug load, formulated as a tablet core coated for gastro-resistant release in the ileum and colon
Implementation Method 2
effectively sequestering bile acids in the colon
Data Source
AI summary
Pharmaceutical compositions comprising bile acid sequestrants, their use in treating bile acid malabsorption, and associated conditions such as bile acid diarrhea and colitis are described herein. Methods for treating bile acid malabsorption and associated conditions are also described.